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Phthalocyanines (Pcs) which have been proposed as sensitizers to supersede haematoporphyrin derivatives, are currently undergoing clinical trials for use in the photo- dynamic therapy (PDT) of cancer . This is due to the superior molar absorptivity of these compounds ,at wavelengths permitting greater penetration of light in normal tissues , when compared with photofrin . Among the unsubstituted phthalocyanines, zinc phthalocyanine has been investigated as a possible second- generation PDT sensitizer. Zinc phthalocyanine itself, because of its water insolubility, is used in liposomal form and has shown sufficient PDT activity . Zinc phthalo- cyanine sulfonic acids have perhaps received the closest attention, and their water solubility is a distinct advantage . Methods for synthesis of sulfonated phthalocyanines, however, often yield complex mixtures composed of different levels of substitution and regioisomers . To overcome such solubility problems, we proposed and synthesized the polyfluoroalkoxyl substituted zinc phthalo- cyanines as sensitizers for PDT. First, the improved solubility of the alkyl-, alkoxyl- or fluorine-substituted phthalocyanines makes their separation and identifion more easy ; second, fluorine is similar in size to hydro- gen and can mimic hydrogen in biological environments . But these quite hydrophobic photosensitizers also need to be bound with cancer-specific antibodies or cyclodextrin dimers for an increase of bioactivity and a decrease of unwanted side reactions . The literature reported preparation procedures are quite intricate. On the other hand, the improved solubility in most organic solvents renders the designated drugs more amenable for formulation in various vehicles, including water–oil emul- sions and nanoparticles and leads to enhanced interaction with membrane . In this report we synthesized tetra(tri- fluoroethoxyl) zinc phthalocyanine , which was used with perfluorocarbon emulsifying agent F68 for photodynamic actions. These studies were performed on myeloma cells and Chinese hamster ovary cells in vitro. |
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茑niao: 金币+20, 翻译EPI+1, ★★★★★最佳答案 2013-05-19 19:47:08
茑niao: 金币+20, 翻译EPI+1, ★★★★★最佳答案 2013-05-19 19:47:08
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酞菁（PCS）已被提议作为敏来取代血卟啉衍生物，目前正在进行临床试验中使用的照片动力疗法（PDT）的癌症。这是由于优越的摩尔吸光系数为这些化合物中，在波长允许更大的渗透在正常组织中的光相比，当与photofrin的。其中的未取代的酞菁，锌酞菁已被研究作为一个可能的第二代PDT增敏剂。锌酞菁本身因为它的水不溶性，以脂质体的形式使用并表现出足够的PDT活动。锌酞菁磺酸也许已经收到最接近 注意，和水溶性是一个明显的优势。磺化酞菁的合成方法，然而，往往产生复杂的混合物组成的的取代和区域异构体的不同的水平。为了克服这样的溶解度问题，我们提出并合成polyfluoroalkoxyl的取代锌酞为PDT敏菁。首先，改进的烷基，烷氧基或氟取代的溶解度酞菁使得他们的分离和identifion的更多容易;第二，氟大小相似，水电在生物环境中的根可以模仿氢。但这些完全疏水性光敏剂也需要绑定与癌特异性抗体或环糊精二聚体的生物活性增加和减少不需要的副反应。文献报告的编写程序是相当复杂的。在另一方面，改进的溶解度大多数有机溶剂呈现指定的药物更适合制定各车辆，包括水油乳化sions和增强互动的纳米粒子，并导致膜。在这份报告中，我们合成的四（三fluoroethoxyl）的酞菁锌，达用全氟化碳乳化剂F68光动力行动。这些究进行 骨髓瘤细胞和中国仓鼠卵巢细胞的体外培养。 |
2楼2013-05-19 17:26:32